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systemic pharmaco > Immunosuppressants > Flashcards

Immunosuppressants Flashcards

1
Q

Uses of immunosuppressants (4)

A
  1. Solid organ/tissue transplantation rejection
  2. Graft vs Host Disease
  3. Autoimmune Diseases (RA, SLE, MS, CD)
  4. Inflammatory Diseases
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2
Q

Classes of immunosuppressants & examples (7)

A
  1. Calcineurin inhibitors (Cyclosporin A, Tacrolimus (FK506) )
  2. mTOR inhibitors (Sirolimus (Rapamycin) )

Cytotoxic agents

  1. Azathioprine
  2. Mycophenolate mofetil (MMF), mycophenolate sodium (MPS)
  3. Polyclonal antibodies (Atgam, thymoglobulin)
  4. Monoclonal antibodies & fusion proteins (Muromonab-CD3 (OKT3) )
  5. Rho (D) immune globulin
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3
Q

Mechanism of action of calcineurin inhibitors

A

T cell-selective immunosuppressants

  1. CSA binds to ubiquitous cytosolic cyclophilin - CSA:cyclophilin complex binds & inhibits calcineurin
  2. Prevents translocation of transcription factor NF-AT - remains phosphorylated, cannot enter nucleus
  3. Inhibits cytokine gene transcription & synthesis
  4. Inhibits primarily T cell proliferation, but also B cell & CTL
  • FK506 binds to ubiquitous cytosolic immunophilin (FKBP)
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4
Q

Uses of calcineurin inhibitors (5)

A
  1. Transplants - kidney, pancreas, liver, cardiac
  2. Uveitis
  3. Rheumatoid Arthritis
  4. Psoriasis
  5. Asthma
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5
Q

Toxicity of calcineurin inhibitors (7)

A
  1. Nephrotoxicity
  2. Hyperglycemia
  3. Hyperlipidemia
  4. Increased cancer risk
  5. Hypertension (CSA)
  6. Gum hyperplasia (CSA)
  7. Neurotoxicity (tacrolimus)
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6
Q

Mechanism of action of mTOR inhibitors

A
  1. Sirolimus binds to FKBP-12 in the cytoplasm - Sirolimus:FKBP complex - binds & inhibits mTOR (Ser/Thr kinase)
  2. Inhibits activity of 70 kDa S6 kinase, activity of 4E-BP1, growth arrest from GI to S phase
  3. Inhibits cytokine-mediated proliferation of T & B cells
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7
Q

Uses of mTOR inhibitors (2)

A
  1. Anti-proliferative & anti-angiogenesis activities

2. Eluting coronary stents to prevent restenosis

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8
Q

Toxicity of mTOR inhibitors (4)

A
  1. Hyperlipidemia
  2. Thrombocytopenia
  3. Delayed wound healing
  4. Mouth ulcers
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9
Q

Mechanism of action of azathioprine

A
  1. Converted to 6-mercaptopurine (6-MP) and then to active metabolite 6-thioguanine (6TG)
  2. Can integrate into DNA
    (A) Structural analog/antimetabolite - impedes DNA synthesis
    (B) formation of thioinosinic acid - inhibits de novo purine synthesis - decreased lymphocyte proliferation
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10
Q

Uses of azathioprine (1)

A
  1. Renal transplant/other autoimmune disorders

- Triple therapy: Steroid + calcineurin inhibitor + azathioprine

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11
Q

Toxicity of azathioprine (2)

A
  1. Bone marrow depression (leukopenia, anemia, thrombocytopenia, bleeding)
  2. Drug interactions: allopurinol inhibits xanthine oxidase which metabolizes 6-MP to an inactive metabolite - accumulation of azathioprine/6-MP - toxicity
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12
Q

Mechanism of action & uses of MMF/MPS

A
  1. Converted to active metabolite mycophenolic acid
  2. Inhibits de novo pathway of purine synthesis by inhibiting inosine 5’-monophosphate dehydrogenase (IMPDH) - preferentially inhibits type II (inducible) over type I (resting)
  • more selective anti-proliferative effects for T/B cells
  • suppresses antibody formation by B cells
  • inhibits recruitment of leukocytes to graft sites
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13
Q

Toxicity of MMF/MPS (4)

A
  1. Diarrhea
  2. Neutropenia
  3. Anemia
  4. Hypertension

less bone marrow depression & GI toxicity than azathioprine

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14
Q

Mechanism of action of polyclonal antibodies

A
  1. Non-selective purified IgG targeted at T & B lymphocytes, NK cells, MHC class I & II antigens, co-stimulatory molecules
  2. Opsonisation & complement dependent cytotoxicity, ADCC, depletion of T-lymphocytes, cross linking of TCR to induce anergy
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15
Q

Uses of polyclonal antibodies

A
  1. Immune globulin intravenous (IGIV) - normalize patients immune network in autoimmune disorders, AIDS, bone marrow transplants
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16
Q

Toxicity of polyclonal antibodies

A
  1. First dose effect - cytokine release syndrome (fever, chill, hypotension), thrombocytopenia, leukopenia, serum sickness, development of anti-foreign IgG antibodies, histiocytic lymphoma at site of injection
17
Q

Mechanism of action of monoclonal antibodies

A

IgG2a subtype directed against CD3-TCR complex, most selective for T lymphocytes - T cell depletion/decreased activity

18
Q

Toxicity of monoclonal antibodies (5)

A
  1. Development of human anti-mouse Ab
  2. Anaphylaxis
  3. Serum sickness
  4. First dose symptoms (cytokine release syndrome)
  5. Increased risk of infection/malignancies
19
Q

Mechanism of action & uses of Rho (D) IgG

A

Human IgG against Rho(D) antigen on RBC

Prevents Rh hemolytic disease of the newborn

  • primary Ab response can be blocked if administered at time of exposure
  • mother’s own Ab response suppressed, disease for next child prevented
20
Q

Toxicity of Rho (D) IgG

A

local discomfort, temperature rise

systemic pharmaco (18 decks)

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